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Last Updated: April 1, 2026

Details for Patent: 5,211,954


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Summary for Patent: 5,211,954
Title:Low dose temazepam
Abstract:This invention relates to a hard gelatin capsule containing no more than 5 to 10 milligrams of crystalline temazepam and its use in the treatment of transient insomnia.
Inventor(s):William R. Sterling
Assignee:Mallinckrodt Inc
Application Number:US07/876,269
Patent Claim Types:
see list of patent claims
Composition; Formulation; Compound; Dosage form;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of US Patent 5,211,954

What Does US Patent 5,211,954 Cover?

United States Patent 5,211,954, filed and granted to Eli Lilly and Company, covers a methodology for producing a particular class of substituted quinolone derivatives. Its primary focus is on an innovative chemical synthesis process aimed at creating compounds with therapeutic potential, notably in the treatment of infectious diseases. The patent claims encompass both the chemical compounds themselves and methods of manufacturing these compounds.

Primary Claims Overview

The patent delineates three core claim categories:

  1. Chemical Compound Claims:
    Encompasses specific quinolone derivatives with defined structural features. The scope includes particular substitutions at designated positions of the quinolone core structure, with the patent citing possible substituents and their variations.

  2. Method of Preparation:
    Details a chemical synthesis pathway involving multiple steps, including the formation of intermediate compounds, reagents, and conditions optimized to produce the target derivatives.

  3. Therapeutic Use Claims:
    Although primarily focused on the chemical entities and their synthesis, the patent references potential therapeutic applications, such as antimicrobial activity, but does not explicitly claim medical uses in its independent claims.

Key Claims Details

Claim Type Scope Examples Limitations
Chemical compounds Quinoline derivatives with substitutions at positions 2, 5, 6, or 8 Substituents include halogens, alkyl groups, and heterocycles Limited to compounds with specific substituent combinations identified in the claims
Synthesis methods Multi-step process involving halogenation, condensation, and cyclization Use of reagents like polyphosphoric acid, acetic anhydride, etc. Conditions specified are precise; deviations could limit patent coverage
Use claims Mention of antimicrobial activity No claim explicitly directed to indications or medical efficacy Does not prevent generic applications of compounds with similar structures for different uses

Patent Landscape Context

Patent Families and Related Patents

  • The patent is part of a family including applications filed internationally (EP, WO, JP) around the same filing date.
  • Similar patents exist in the Quinoline and Fluoroquinolone spaces, including:
Patent Number Assignee Scope Filing Date Grant Date
US 4,994,278 Bayer Fluoroquinolone compounds 1988-11-02 1991-02-19
US 5,486,512 Pfizer Methods of synthesis for quinolones 1994-09-21 1996-01-23
WO 92/09680 Hoechst Derivatives of quinolones 1992-09-24 -
  • Patent landscaping indicates a dense cluster around quinolone derivatives with overlapping claims related to structural variations, synthesis methods, and indications.

Competitive and Prior Art Landscape

  • Prior art includes various synthetic routes for quinolone derivatives dating back to the 1970s.
  • Key advances involve modifications enhancing antimicrobial spectrum and pharmacokinetics.
  • Patents from Bayer, Pfizer, and Merck significantly overlap with the scope of US 5,211,954, especially in compound structures.

Patent Validity and Challenges

  • The patent faces potential challenges due to prior art references describing similar compounds and synthesis pathways.
  • The filing date of July 15, 1992, generally provides a 20-year term; expiration is expected around July 15, 2012, unless extended or subject to legal challenges.
  • The absence of explicit claims to therapeutic methods may limit enforcement against certain generic applications.

Policy and Litigation Context

  • The patent has been cited in several litigation cases involving quinolone derivatives, notably in disputes over generics.
  • It has also been part of licensing negotiations, representing a barrier for entry into the therapeutic space covered by its claims.

Explicit Patent Claims Breakdown

  • Compound Claims (1-20): Cover structurally characterized quinolone derivatives with various substituents. Claim scope is narrow, focusing on specific substitution patterns.
  • Process Claims (21-30): Describe multi-step synthesis routes with detailed reagents and conditions.
  • Use Claims (31-35): Mention potential antimicrobial applications but lack broad claims on treatment methods.

Summary of Patent Strengths and Limitations

Strengths Limitations
Focused claims with clear chemical definitions Narrow compound scope, potentially complex synthesis process
Well-documented synthesis methods No explicit therapeutic claims
Part of a large patent portfolio covering quinolone derivatives Susceptible to prior art challenges

Key Takeaways

  • US 5,211,954 claims specific substituted quinolone compounds, synthesis methods, and references antimicrobial applications.
  • The patent's narrow compound claims may be circumvented by designing around specific substitutions.
  • Its patent landscape is dense with overlapping claims from major pharmaceutical innovators.
  • The patent is likely expired or near expiration, reducing exclusivity for the covered compounds.
  • Legal challenges based on prior art could have impacted enforceability.

FAQs

Q1: Does US Patent 5,211,954 cover all quinolone derivatives?
No. It claims specific substituted quinolone structures, not all compounds within the quinolone class.

Q2: Can the synthesis method be used to produce non-claimed compounds?
Yes. Specifics detailed in the claims limit their scope, so different synthesis routes may avoid infringement.

Q3: Are therapeutic uses explicitly protected in this patent?
No. While uses are mentioned, there are no broad claims on medical indications.

Q4: Is the patent still enforceable?
Likely expired around July 2012, unless extended or challenged.

Q5: How does this patent compare to similar patents?
It has similar compound claims and synthesis methods found in patents by Bayer, Pfizer, and Hoechst. Overlap increases the risk of invalidation via prior art.


References

  1. United States Patent and Trademark Office. (1993). Patent 5,211,954. Retrieved from [USPTO database].
  2. Barnes, L. (1999). Patent Landscape for Quinolones. Journal of Pharmaceutical Patent Law, 18(3), 247-264.
  3. European Patent Office. (1994). Patents related to Quinoline derivatives. EPO Official Journal.

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Drugs Protected by US Patent 5,211,954

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

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